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  3. CHIR-99021 trihydrochloride

CHIR-99021 trihydrochloride (Synonyms: CT99021 trihydrochloride)

Cat. No.: HY-10182B Purity: 97.93%
Handling Instructions

CHIR-99021 trihydrochloride (CT99021 trihydrochloride) is a GSK-3α/β inhibitor with IC50 of 10 nM/6.7 nM; >500-fold selectivity for GSK-3 versus its closest homologs CDC2 and ERK2, as well as other protein kinases.

For research use only. We do not sell to patients.

CHIR-99021 trihydrochloride Chemical Structure

CHIR-99021 trihydrochloride Chemical Structure

CAS No. : 1782235-14-6

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 121 In-stock
Estimated Time of Arrival: December 31
5 mg USD 96 In-stock
Estimated Time of Arrival: December 31
10 mg USD 156 In-stock
Estimated Time of Arrival: December 31
50 mg USD 588 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 37 publication(s) in Google Scholar

Other Forms of CHIR-99021 trihydrochloride:

Top Publications Citing Use of Products

    CHIR-99021 trihydrochloride purchased from MCE. Usage Cited in: Toxicology. 2016 May 20;355-356:31-38.

    Western analysis of β-catenin protein level in zebrafish embryos exposed to EOM in the presence or absence of CH/CHIR (n = 3). Different letters indicate significant differences. Moreover, both CH and CHIR attenuate the EOM-induced changes in the protein level of b-catenin and in EROD activity.

    CHIR-99021 trihydrochloride purchased from MCE. Usage Cited in: Chemosphere. 2018 Oct 23;216:372-378.

    AhR mediates EOM-inhibited cardiac differentiation by downregulating β-catenin expression in P19 cells. mRNA expression changes of β-catenin by Q-PCR. The concentrations of CH (CH223191, AhR antagonist) and CHIR (CHIR99021, Wnt activator) are 0.25 and 0.5 μM respectively.

    CHIR-99021 trihydrochloride purchased from MCE. Usage Cited in: Chemosphere. 2018 Oct 23;216:372-378.

    AhR mediates EOM-inhibited cardiac differentiation by downregulating β-catenin expression in P19 cells. Percentage of cTnT positive cells at differentiation day 14. The concentrations of CH (CH223191, AhR antagonist) and CHIR (CHIR99021, Wnt activator) are 0.25 and 0.5 μM respectively.

    CHIR-99021 trihydrochloride purchased from MCE. Usage Cited in: Chemosphere. 2018 Oct 23;216:372-378.

    AhR mediates EOM-inhibited cardiac differentiation by downregulating β-catenin expression in P19 cells. Percentage of cTnT positive cells at differentiation day 14. The concentrations of CH (CH223191, AhR antagonist) and CHIR (CHIR99021, Wnt activator) are 0.25 and 0.5 μM respectively.

    CHIR-99021 trihydrochloride purchased from MCE. Usage Cited in: Biochem Biophys Res Commun. 2020 Jan 24. pii: S0006-291X(20)30143-1.B

    Western blot analysis of Tcf7l1 protein levels in mESCs pre-treated with the indicative different small molecules for 1 h and then treated with CHIR for 24 h.

    CHIR-99021 trihydrochloride purchased from MCE. Usage Cited in: Biochem Biophys Res Commun. 2020 Jan 24. pii: S0006-291X(20)30143-1.B

    Western blot analysis of Tcf7l1 protein levels in mESCs pre-treated with D4476 or DMAT and then treated with CHIR or PD03 for 24 h.

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    Description

    CHIR-99021 trihydrochloride (CT99021 trihydrochloride) is a GSK-3α/β inhibitor with IC50 of 10 nM/6.7 nM; >500-fold selectivity for GSK-3 versus its closest homologs CDC2 and ERK2, as well as other protein kinases.

    IC50 & Target[1]

    GSK-3β

    6.7 nM (IC50)

    GSK-3α

    10 nM (IC50)

    cdc2

    8800 nM (IC50)

    In Vitro

    CHIR-99021 inhibits human GSK-3β with Ki values of 9.8 nM[1]. CHIR-99021 is a small organic molecule that inhibits GSK3α and GSK3β by competing for their ATP-binding sites.In vitro kinase assays reveal that CHIR-99021 specifically inhibits GSK3β (IC50=~5 nM) and GSK3α (IC50=~10 nM), with little effect on other kinases[2]. In the presence of CHIR-99021 the viability of the ES-D3 cells is reduced by 24.7% at 2.5 μM, 56.3% at 5 μM, 61.9% at 7.5 μM and 69.2% at 10 μM CHIR-99021 with an IC50 of 4.9 μM[3].

    In Vivo

    In ZDF rats, a single oral dose of CHIR-99021 (16 mg/kg or 48 mg/kg) rapidly lowers plasma glucose, with a maximal reduction of nearly 150 mg/dl 3-4 h after administration[1]. CHIR99021 (2 mg/kg) given once, 4 h before irradiation, significantly improves survival after 14.5 Gy abdominal irradiation (ABI). CHIR99021 treatment significantly blocks crypt apoptosis and accumulation of p-H2AX+ cells, and improves crypt regeneration and villus height. CHIR99021 treatment increases Lgr5+ cell survival by blocking apoptosis, and effectively prevents the reduction of Olfm4, Lgr5 and CD44 as early as 4 h[4].

    Molecular Weight

    574.72

    Formula

    C₂₂H₂₁Cl₅N₈

    CAS No.

    1782235-14-6

    SMILES

    N#CC1=CC=C(NCCNC2=NC=C(C3=NC=C(C)N3)C(C4=CC=C(Cl)C=C4Cl)=N2)N=C1.[H]Cl.[H]Cl.[H]Cl

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 32 mg/mL (55.68 mM)

    H2O : 19 mg/mL (33.06 mM; Need ultrasonic and warming)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.7400 mL 8.6999 mL 17.3998 mL
    5 mM 0.3480 mL 1.7400 mL 3.4800 mL
    10 mM 0.1740 mL 0.8700 mL 1.7400 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.58 mg/mL (4.49 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.58 mg/mL (4.49 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.58 mg/mL (4.49 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
    Cell Assay
    [3]

    The viability of the mouse ES cells is determined after exposure to different concentrations of GSK3 inhibitors for three days using the MTT assay. The decrease of MTT activity is a reliable metabolism-based test for quantifying cell viability; this decrease correlates with the loss of cell viability. 2,000 cells are seeded overnight on gelatine-coated 96-well plates in LIF-containing ES cell medium. On the next day the medium is changed to medium devoid of LIF and with reduced serum and supplemented with 0.1-1 μM BIO, or 1-10 μM SB-216763, CHIR-99021 or CHIR-98014. Basal medium without GSK3 inhibitors or DMSO is used as control. All tested conditions are analyzed in triplicates[3].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [1][4]

    Rats[1]
    Primary hepatocytes from male Sprague Dawley rats that weighed <140 g are prepared and used 1-3 h after isolation. Aliquots of 1×106cells in 1 mL of DMEM/F12 medium plus 0.2% BSA and CHIR-99021(orally at 16 or 48 mg/kg) or controls are incubated in 12-well plates on a low-speed shaker for 30 min at 37°C in a CO2-enriched atmosphere, collected by centrifugation and lysed by freeze/thaw in buffer A plus 0.01% NP40; the GS assay is again performed.
    Mice[4]
    Mice 6-10 weeks old are used. The PUMA+/+ and PUMA-/- littermates on C57BL/6 background (F10) and Lgr5-EGFP (Lgr5-EGFP-IRES-creERT2) mice are subjected to whole body irradiation (TBI), or abdominal irradiation (ABI). Mice are injected intraperitoneally (i.p.) with 2 mg/kg of CHIR99021 4 h before radiation or 1 mg/kg of SB415286 28 h and 4 h before radiation. Mice are sacrificed to collect small intestines for histology analysis and western blotting. All mice are injected i.p. with 100 mg/kg of BrdU before sacrifice.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
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    Keywords:

    CHIR-99021 trihydrochlorideCT99021 trihydrochlorideGSK-3AutophagyGlycogen synthase kinase-3Glycogen synthase kinase 3Inhibitorinhibitorinhibit

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    CHIR-99021 trihydrochloride
    Cat. No.:
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